At Least Three Nitrogens In The Hetero Ring Patents (Class 540/501)
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Patent number: 8895545Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: October 4, 2012Date of Patent: November 25, 2014Assignee: Debiopharm International SAInventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20140275019Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHDInventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
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Publication number: 20140107106Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: April 25, 2013Publication date: April 17, 2014Applicant: Affinium Pharmaceuticals, Inc.Inventor: Affinium Pharmaceuticals, Inc.
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Publication number: 20130345206Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Patent number: 8592577Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims. Additionally, the present invention relates to compounds of Structural Formula (I), which are useful as inhibitors of protein kinase.Type: GrantFiled: March 20, 2012Date of Patent: November 26, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant, Michael O'Donnell
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Publication number: 20130150350Abstract: Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: February 9, 2011Publication date: June 13, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bruno Simoneau, Patrick Deroy, Lee Fader, Anne-Marie Faucher, Alexander Gagnon, Chantal Grand-Maitre, Stephen Kawai, Serge Landry, Jean-Francois Mercier, Jean Rancourt
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Patent number: 8394952Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 10, 2011Date of Patent: March 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Kay, Ronald Knetgel, Jean-Damien Charrier, Heather Twin
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Patent number: 8318720Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: July 19, 2007Date of Patent: November 27, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20120178915Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: December 24, 2009Publication date: July 12, 2012Inventor: Lifeng Xu
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Publication number: 20120165319Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.Type: ApplicationFiled: November 10, 2011Publication date: June 28, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M.C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L.C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 8202990Abstract: The present invention relates generally to processes of making 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide and Form A of 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide.Type: GrantFiled: September 25, 2008Date of Patent: June 19, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Christopher McBride, Zhe Nie
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Patent number: 8188116Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.Type: GrantFiled: July 13, 2007Date of Patent: May 29, 2012Assignee: Vanderbilt UniversityInventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
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Publication number: 20120129846Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: May 24, 2012Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
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Publication number: 20120108575Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: ApplicationFiled: January 12, 2012Publication date: May 3, 2012Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.Inventors: Kevin C. Brown, R, Richard Goehring, Yoshiyasu BABA, Naoki Tsuno
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Publication number: 20120088770Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: May 7, 2010Publication date: April 12, 2012Applicant: Prism BioLab CorporationInventors: Takenao Odagami, Yiji Kogami, Hiroyuki Kouji
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Patent number: 8119631Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.Type: GrantFiled: May 24, 2010Date of Patent: February 21, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 8022202Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: September 29, 2009Date of Patent: September 20, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
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Patent number: 8012960Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 7, 2010Date of Patent: September 6, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Patent number: 8003785Abstract: The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.Type: GrantFiled: June 16, 2009Date of Patent: August 23, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Jianping Cai, Shaoqing Chen, Xin-Jie Chu, Kin-Chun Luk, Steven Gregory Mischke, Hongmao Sun, Peter Michael Wovkulich
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Publication number: 20110082111Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 7, 2010Publication date: April 7, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Patent number: 7838517Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 15, 2009Date of Patent: November 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20100278739Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.Type: ApplicationFiled: July 13, 2010Publication date: November 4, 2010Inventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
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Publication number: 20100247519Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: June 7, 2010Publication date: September 30, 2010Applicant: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Publication number: 20100069333Abstract: The invention provides ?-mimetic structures and a chemical library relating thereto. Additionally, the invention provides methods wherein ?-mimetic compounds are used to treat cancer stem cells.Type: ApplicationFiled: November 11, 2009Publication date: March 18, 2010Applicant: Choongwae Pharma CorporationInventor: Michael Kahn
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Publication number: 20100022519Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Kevin C. Brown, R. Richard Goehring, Yoshiyasu Baba, Naoki Tsuno
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Patent number: 7622463Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: February 13, 2007Date of Patent: November 24, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
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Patent number: 7582753Abstract: The present invention is directed to a novel process for the preparation of benzo[e][1,2,4]triazepin-2-one derivatives, useful in the preparation of gastrin and cholecystokinin receptor ligands.Type: GrantFiled: September 14, 2006Date of Patent: September 1, 2009Assignee: JanssenPharmaceutica, NVInventors: Ahmed F. Abdel-Magid, Luigi Anzalone, Judith Cohen, Steven Mehrman, Frank Villani
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Publication number: 20090215781Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.Type: ApplicationFiled: March 15, 2006Publication date: August 27, 2009Applicant: INSTITUTE FOR CHEMICAL GENOMICSInventors: Michael Kahn, Masakatsu Eguchi
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Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
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Patent number: 7524837Abstract: This invention relates to pharmaceutically acceptable salts of compounds of formula (I) Such salts are useful, for example, for the treatment of gastrin related disorders.Type: GrantFiled: April 27, 2004Date of Patent: April 28, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen
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Patent number: 7517873Abstract: The present invention provides PLK1 inhibitor compounds of formula I: Useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas.Type: GrantFiled: March 19, 2008Date of Patent: April 14, 2009Assignee: Hoffman-La Roche Inc.Inventor: Shaoqing Chen
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Publication number: 20090005359Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: June 30, 2008Publication date: January 1, 2009Applicant: Sunesis Pharmaceuticals, IncInventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Patent number: 7186828Abstract: A method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, includes a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of the carbamic acid derivative(s).Type: GrantFiled: June 13, 2001Date of Patent: March 6, 2007Assignee: ImmuPharma (France) SAInventors: Gilles Guichard, Marie-Christine Galas-Rodriguez, legal representative, Pierre Rodriguez, legal representative, Elisa Rodriguez, legal representative, Romain Rodriguez, legal representative, Serge Plaue, Vincent Semetey, Arnaud-Pierre Schaffner, Jean-Paul Briand, Marc Rodriguez, deceased
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Patent number: 6962912Abstract: The invention relates to novel substituted pyrazolo[4,3-e]-diazepines of general formula: to pharmaceutical compositions containing them, to their use as medicinal products and to processes for preparing them.Type: GrantFiled: December 27, 2000Date of Patent: November 8, 2005Assignee: Warner-Lambert LLCInventors: Catherine Burnouf, Amaya Berecibar, Michael Navet
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Patent number: 6943157Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a and R3 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.Type: GrantFiled: October 9, 2002Date of Patent: September 13, 2005Assignee: Myriad Genetics, Inc.Inventors: Gangadhar Nagula, Jan Urban, Hwa-Ok Kim, Christopher Lum, Hiroshi Nakanishi
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Patent number: 6867298Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: GrantFiled: May 8, 2003Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Patent number: 6825191Abstract: The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.Type: GrantFiled: March 27, 2003Date of Patent: November 30, 2004Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Munetaka Tokumasu, Kazumi Tashiro, Mitsuo Takahashi, Takashi Kayahara, Shunji Takehana, Yuki Kajigaya, Kaoru Yoshida, Kuniya Sakurai
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Patent number: 6821993Abstract: This invention relates to a series of triazepines of Formula I and II, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treatment and prevention of neuronal disorders such as Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis diabetic neuropathy and Bell's palsy.Type: GrantFiled: October 4, 2002Date of Patent: November 23, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Zhihua Sui, Shawn P. Walsh
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Publication number: 20040048855Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: ApplicationFiled: April 25, 2003Publication date: March 11, 2004Applicant: Vertex Pharmaceuticals IncorporatedInventors: Julian M .C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L.C. Robidoux, Marion W. Wannamaker
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Publication number: 20030186969Abstract: The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.Type: ApplicationFiled: March 27, 2003Publication date: October 2, 2003Applicant: AJINOMOTO CO. INCInventors: Tadakiyo Nakagawa, Munetaka Tokumasu, Kazumi Tashiro, Mitsuo Takahashi, Takashi Kayahara, Shunji Takehana, Yuki Kajigaya, Kaoru Yoshida, Kuniya Sakurai
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Patent number: 6573259Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: October 23, 2001Date of Patent: June 3, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L. C. Robidoux, Marion W. Wannamaker
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Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
Patent number: 6452001Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;Type: GrantFiled: May 14, 2001Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck -
Publication number: 20020115854Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: ApplicationFiled: December 4, 2001Publication date: August 22, 2002Inventors: Patrick Y.S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J.P. Pinto, Ruth R. Wexler
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Patent number: 6426413Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: September 5, 2000Date of Patent: July 30, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Paul Charifson, David J. Lauffer, Michael D. Mullican
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Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
Publication number: 20020010174Abstract: The invention relates to compounds of the formula 1Type: ApplicationFiled: May 14, 2001Publication date: January 24, 2002Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck -
Patent number: 6258948Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.Type: GrantFiled: September 21, 1999Date of Patent: July 10, 2001Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 5874424Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: February 8, 1996Date of Patent: February 23, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Robert E. Zelle
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Patent number: 5869487Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##Type: GrantFiled: October 24, 1997Date of Patent: February 9, 1999Assignee: Merck & Co., Inc.Inventors: Craig Coburn, Christine Kolatac, Diane M. Rush, Joseph P. Vacca
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Patent number: 5807850Abstract: Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula ?I! ##STR1## wherein R.sup.1 is aryl or heteroaryl; R.sup.2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R.sup.4 is hydrogen atom or halogen atom, or R.sup.2 and R.sup.4 form carbonyl combinedly together with the carbon atom to which they bond; R.sup.3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, --X--Y wherein X is --(CH.sub.2).sub.m --, --CO--, --COCH.sub.2 --, --NH--, --NHCH.sub.2 --, --CH.sub.2 NH--, --CH.sub.2 NHCO--, --OCH.sub.2 --, --(CH.sub.2).sub.n O-- or --CH.sub.2 S-- and Y is halogen atom, cycloallyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula ?I! have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.Type: GrantFiled: May 5, 1997Date of Patent: September 15, 1998Assignee: Japan Tobacco, Inc.Inventors: Takeshi Nakamura, Yoshihisa Koga, Masanori Shindo